Tclin EPHA2 Ephrin type-A receptor 2

Protein Summary

Description

Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Activated by the ligand ephrin-A1/EFNA1 regulates migration, integrin-mediated adhesion, proliferation and differentiation of cells. Regulates cell adhesion and differentiation through DSG1/desmoglein-1 and inhibition of the ERK1/ERK2 (MAPK3/MAPK1, respectively) signaling pathway. May also participate in UV radiation-induced apoptosis and have a ligand-independent stimulatory effect on chemotactic cell migration. During development, may function in distinctive aspects of pattern formation and subsequently in development of several fetal tissues. Involved for instance in angiogenesis, in early hindbrain development and epithelial proliferation and branching morphogenesis during mammary gland development. Engaged by the ligand ephrin-A5/EFNA5 may regulate lens fiber cells shape and interactions and be important for lens transparency development and maintenance. With ephrin-A2/EFNA2 may play a role in bone remodeling through regulation of osteoclastogenesis and osteoblastogenesis. (Microbial infection) Acts as a receptor for hepatitis C virus (HCV) in hepatocytes and facilitates its cell entry. Mediates HCV entry by promoting the formation of the CD81-CLDN1 receptor complexes that are essential for HCV entry and by enhancing membrane fusion of cells expressing HCV envelope glycoproteins. This gene belongs to the ephrin receptor subfamily of the protein-tyrosine kinase family. EPH and EPH-related receptors have been implicated in mediating developmental events, particularly in the nervous system. Receptors in the EPH subfamily typically have a single kinase domain and an extracellular region containing a Cys-rich domain and 2 fibronectin type III repeats. The ephrin receptors are divided into 2 groups based on the similarity of their extracellular domain sequences and their affinities for binding ephrin-A and ephrin-B ligands. This gene encodes a protein that binds ephrin-A ligands. Mutations in this gene are the cause of certain genetically-related cataract disorders.[provided by RefSeq, May 2010]

Uniprot Accession IDs

• P29317
• B5A968
• Q8N3Z2

Gene Name

• EPHA2

Ensembl ID

• ENST00000358432
• ENSP00000351209
• ENSG00000142627

Symbol

• ECK
• ECK
• CTPA
• ARCC2
• CTPP1
• CTRCT6

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
protein domain	1
molecular function	0.98
PubMedID	0.98
biological process	0.95
interacting protein	0.85

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Tk Group / Eph Family / Ephrin Type-a Receptor 2

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 821.74   (req: < 5)

Gene RIFs: 212   (req: <= 3)

Antibodies: 1179   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 821.74   (req: >= 5)

Gene RIFs: 212   (req: > 3)

Antibodies: 1179   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 52

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 47

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 3

Expression Data (0 Tissues)

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No expression data found

Protein Sequence and Structure

Residue Counts

Protein Sequence

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Related Tools (5)

ProKinO

The ProKinO is a protein kinase-specific ontology, which provides a controlled vocabulary of terms, their hierarchy, and relationships unifying sequence, structure, function, mutation and pathway information on kinases.

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Target Illumination GWAS Analytics (TIGA)

TIGA scores and ranks GWAS discovered associations according to the quantity and quality of the evidence supporting the association.

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GENEVA

GENEVA (GENe Expression Variance Analysis) allows you to identify RNA-sequencing datasets from the Gene Expression Omnibus (GEO) that contain conditions modulating a gene or a gene signature.

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GlyGen

GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.

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ARCHS4

ARCHS4 provides access to gene-function predictions based on RNA-seq co-expression, and gene expression levels across cell and tissues.

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Approved Drugs (3)

Explore Approved Drugs

1 – 3 of 3

bosutinib

EPHA2Tclin Kinase

INHIBITOR pKd : 8.38

dasatinib

EPHA2Tclin Kinase

INHIBITOR pKd : 7.89

ponatinib

EPHA2Tclin Kinase

INHIBITOR pKi : 8.8

Active Ligands (47)

Explore Active Ligands

1 – 10 of 47

foretinib

EPHA2Tclin Kinase

pKd : 7.92

SID103904591

EPHA2Tclin Kinase

pKi : 7.8

PD-173955

EPHA2Tclin Kinase

pKd : 7.92

TG-100572

EPHA2Tclin Kinase

pKd : 9.05

SID103904326

EPHA2Tclin Kinase

pKi : 8.4

SID103904313

EPHA2Tclin Kinase

pKi : 7.9

SID103904320

EPHA2Tclin Kinase

pKi : 7.7

CHEMBL249097

EPHA2Tclin Kinase

pKd : 8.3

SID103904289

EPHA2Tclin Kinase

pKi : 7.9

CHEMBL1784637

EPHA2Tclin Kinase

pIC50 : 9.7

Protein-Protein Interactions (276)

Explore Interacting Targets

1 – 10 of 276

• See Interactions on String-DB

SDC1

Tbio

Novelty:  0.00044792

p_int:  0.998340724

p_ni:  0.001659276

Score:  0.414

Data Source:  BioPlex,STRINGDB

EFNA5

Tbio

Novelty:  0.00134985

p_int:  0.997568562

p_ni:  0.002431438

Score:  0.999

Data Source:  BioPlex,STRINGDB

CYP2S1

Tbio

Novelty:  0.02967417

p_int:  0.98670038

p_ni:  0.013299617

p_wrong:  3e-9

Score:  0.155

Data Source:  BioPlex,STRINGDB

CCR1

Tchem

Family:  GPCR

Novelty:  0.00218065

p_int:  0.930026402

p_ni:  0.069694096

p_wrong:  0.000279502

Score:  0.212

Data Source:  BioPlex,STRINGDB

GJB7

Tbio

Novelty:  0.12555147

p_int:  0.923252667

p_ni:  0.076747331

p_wrong:  2e-9

Data Source:  BioPlex

LRRIQ1

Tdark

Novelty:  1.8251367

p_int:  0.899352611

p_ni:  0.100394209

p_wrong:  0.00025318

Score:  0.194

Data Source:  BioPlex,STRINGDB

NCSTN

Tbio

Novelty:  0.00453935

p_int:  0.868744829

p_ni:  0.131038183

p_wrong:  0.000216987

Data Source:  BioPlex

NTRK3

Tclin

Family:  Kinase

Novelty:  0.00177321

p_int:  0.851152407

p_ni:  0.14884376

p_wrong:  0.000003833

Score:  0.177

Data Source:  BioPlex,STRINGDB

MAS1

Tchem

Family:  GPCR

Novelty:  0.0089712

p_int:  0.842168969

p_ni:  0.157830376

p_wrong:  6.55e-7

Score:  0.154

Data Source:  BioPlex,STRINGDB

SLC25A41

Tdark

Family:  Transporter

Novelty:  1.04918395

p_int:  0.84216459

p_ni:  0.153363658

p_wrong:  0.004471752

Data Source:  BioPlex

Nearest Tclin Targets

Nearest Tclin calculations are only available for targets with KEGG Pathway annotations.

Pathways (30)

Reactome (4)

KEGG (5)

PathwayCommons (7)

WikiPathways (14)

Axon guidance (R-HSA-422475)

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1 – 4 of 4

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Axon guidance	533 targets	R-HSA-422475
Reactome	Developmental Biology	1055 targets	R-HSA-1266738
Reactome	EPH-Ephrin signaling	92 targets	R-HSA-2682334
Reactome	EPH-ephrin mediated repulsion of cells	49 targets	R-HSA-3928665

Name	Explore in Pharos	Explore in Source
Axon guidance	533 targets	R-HSA-422475
Developmental Biology	1055 targets	R-HSA-1266738
EPH-Ephrin signaling	92 targets	R-HSA-2682334
EPH-ephrin mediated repulsion of cells	49 targets	R-HSA-3928665

Viral Interactions (0)

No viral interactions found

Gene Ontology Terms (64)

Functions (6)

Components (12)

Processes (46)

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1 – 6 of 6

GO Term	Evidence	Assigned by
transmembrane receptor protein tyrosine kinase activity	Inferred from Direct Assay (IDA)	UniProtKB
cadherin binding	Inferred from High Throughput Direct Assay (HDA)	BHF-UCL
transmembrane signaling receptor activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
transmembrane-ephrin receptor activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
ATP binding	Inferred from Electronic Annotation (IEA)	UniProtKB-KW
virus receptor activity	Inferred from Electronic Annotation (IEA)	UniProtKB-KW

Disease Associations (null)

No disease associations found

GWAS Traits (26)

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5

1 – 5 of 26

GWAS Trait	EFO ID	Study Count	SNP Count	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
serum gamma-glutamyl transferase measurement	EFO_0004532	7	15	18	3.8	99.8
low density lipoprotein cholesterol measurement	EFO_0004611	5	3	5		92.4
aspartate aminotransferase measurement	EFO_0004736	2	2	1	13.2	84.6
hematocrit	EFO_0004348	3	3	3		83.9
hemoglobin measurement	EFO_0004509	3	3	3		82.9

• Explore on Target Illumination GWAS Analytics (TIGA)

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5

1 – 5 of 26

GWAS Trait	EFO ID	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
serum gamma-glutamyl transferase measurement	EFO_0004532	18	3.8	99.8
low density lipoprotein cholesterol measurement	EFO_0004611	5		92.4
aspartate aminotransferase measurement	EFO_0004736	1	13.2	84.6
hematocrit	EFO_0004348	3		83.9
hemoglobin measurement	EFO_0004509	3		82.9

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Find similar targets by:

UniProt Keyword Find Similar Targets

No Header	No Header
3D-structure
Alternative splicing
Angiogenesis
Apoptosis
ATP-binding
Cataract
Cell adhesion
Cell junction
Cell membrane
Cell projection

GWAS Trait Find Similar Targets

No Header	No Header
apolipoprotein B measurement
appendicular lean mass
aspartate aminotransferase measurement
balding measurement
blood protein measurement
blood urea nitrogen measurement
brain measurement
calcium measurement
cortical thickness
erythrocyte count

MGI Phenotype Find Similar Targets

No Header	No Header
cardiovascular system phenotype
embryo phenotype
homeostasis/metabolism phenotype
limbs/digits/tail phenotype
neoplasm
nervous system phenotype
skeleton phenotype
vision/eye phenotype

IDG Resources

No IDG generated resources found

Orthologs (11)

1 – 5 of 11

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Chimp	EPH receptor A2	VGNC:531	456472
Macaque	EPH receptor A2		692343
Mouse	Eph receptor A2	MGI:95278	13836
Rat	Eph receptor A2	RGD:1307204	366492
Dog	EPH receptor A2	VGNC:40405	487421

Species	Name	OMA	EggNOG	Inparanoid
Chimp	EPH receptor A2
Macaque	EPH receptor A2
Mouse	Eph receptor A2
Rat	Eph receptor A2
Dog	EPH receptor A2

Publication Statistics

PubMed Score 821.74

PubMed score by year

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PubTator Score 377.54

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Patents

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Text Mined References (256)

GeneRif Annotations (212)

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PMID	Year	Title